Drug intelligence / Profile preview

LG1-137

Development stage
Discontinued
Lead developer
Emory University
Modality
Small Molecules
01

Overview

LG1-137 is a small molecule research tool and an inactive analog of the EYA2 inhibitor LG1-34. Developed through a collaboration between Emory University and the University of Colorado, it is specifically designed with a significantly reduced binding affinity for the Eyes Absent 2 (EYA2) protein tyrosine phosphatase compared to its active counterpart. In preclinical studies focusing on SIX1-expressing pediatric leukemias, such as Acute Myeloid Leukemia (AML) and T-cell Acute Lymphoblastic Leukemia (T-ALL), LG1-137 serves as a negative control to validate that the anti-proliferative effects of EYA2 inhibitors are due to the specific inhibition of the EYA2 phosphatase activity. Experimental data indicates that LG1-137 has minimal impact on leukemia cell proliferation, with IC50 values approximately 30 to 90 times higher than those of the potent inhibitor LG1-34.

02

Targets

EYA2 (Eyes absent homolog 2)

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